ER-α36 is a recently discovered estrogen receptor, predominantly located on the plasma membrane and in the cytoplasm, that is found to mediate membrane-initiated “non-genomic” signaling pathways. The membrane-initiated signal has been acknowledged as a fast response signal related to estrogen, and usually activates the signaling pathway such as MAPK/ERK, phosphatidylinositol 3-kinase and protein kinase C. Pre-clinical experiments disclose that ER-α36 expression in tumor cells appears to drive the propagation of breast cancer cells. Further, ER-α36 has been found to be expressed in many cancers, and plays an important role in cancer and tumor progression.
Icaritin, referring to the formula (I), is a new and effective monomer obtained by the enzyme hydrolysis of Icariin, which is an active ingredient isolated from Epimedium Herb.

Icaritin is disclosed in China patent ZL.200780039276.9 for the treatment of diseases related to the abnormal proliferation of estrogen receptor cells expressing ER-α36, wherein the diseases comprise several varieties of cancers.
The method of preparing Icaritin is disclosed in CN101302548B. In this method, Icariin, as a starting material, is hydrolyzed with β-D-Glucosidase, centrifuged, and the pellet obtained from centrifugating the hydrolysis product is dissolved with acetone. Following a second centrifugation and filtration, the supernatant is collected. Pure Icaritin is obtained after recrystalizing the supernatant.
There is no report about administrating Icaritin to a subject in the prior art.